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floxuridine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| uridine derivatives used as antiviral agents and as antineoplastics | 1184 | 50-91-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 24.62 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PRKDC,TEK | 18 | |||
| kinase-selectivity-class | AXL,CDK9,GRK2,IRAK1,MAP3K14,PDK1,PRKDC | 7 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | Moderate | 0.76 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 18, 1970 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01BC09 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Pyrimidine analogues |
| FDA CS | M0006020 | Deoxyuridine |
| MeSH PA | D000963 | Antimetabolites |
| MeSH PA | D000964 | Antimetabolites, Antineoplastic |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA EPC | N0000180853 | Antimetabolite |
| CHEBI has role | CHEBI:35221 | antimetabolite |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:36044 | antiviral drug |
| CHEBI has role | CHEBI:132992 | radiosensitizing agent |
Related Drugs by ATC class:
L01BC Pyrimidine analogues 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malignant neoplasm of liver | indication | 93870000 | DOID:3571 |
| Primary malignant neoplasm of gastrointestinal tract | indication | 363745004 | |
| Nutritional disorder | contraindication | 2492009 | DOID:374 |
| Acute hemorrhage | contraindication | 8573003 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Esophagitis | contraindication | 16761005 | DOID:11963 |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Fibrosis of bile duct | contraindication | 48124008 | |
| Stomatitis | contraindication | 61170000 | DOID:9637 |
| Acute infectious disease | contraindication | 63171007 | |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Cholecystitis | contraindication | 76581006 | DOID:1949 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Liver function tests abnormal | contraindication | 166603001 | |
| Persistent vomiting | contraindication | 196746003 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Bone marrow depression | contraindication | 307762000 | |
| Pharyngitis | contraindication | 405737000 | DOID:2275 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.98 | acidic |
| pKa2 | 13.02 | acidic |
| pKa3 | 13.7 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Thymidylate synthase | Enzyme | INHIBITOR | DRUGBANK | CHEMBL | |||||
| Thymidylate synthase | Enzyme | IC50 | 9.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017811 | VUID |
| N0000146171 | NUI |
| D04197 | KEGG_DRUG |
| 4017811 | VANDF |
| C0016343 | UMLSCUI |
| CHEBI:60761 | CHEBI |
| CHEMBL917 | ChEMBL_ID |
| DB00322 | DRUGBANK_ID |
| D005467 | MESH_DESCRIPTOR_UI |
| 5790 | PUBCHEM_CID |
| 4801 | IUPHAR_LIGAND_ID |
| 2010 | INN_ID |
| 039LU44I5M | UNII |
| 4488 | RXNORM |
| 40527 | MMSL |
| 4731 | MMSL |
| d01344 | MMSL |
| 002648 | NDDF |
| 387432008 | SNOMEDCT_US |
| 75927008 | SNOMEDCT_US |
| 039LU44I5M | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Floxuridine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9270 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 100 mg | INTRA-ARTERIAL | ANDA | 24 sections |
| Floxuridine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63323-145 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 500 mg | INTRA-ARTERIAL | ANDA | 13 sections |
| Floxuridine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 81643-9270 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 500 mg | INTRA-ARTERIAL | ANDA | 24 sections |